JP2004530721A5

JP2004530721A5 -

Info

Publication number: JP2004530721A5
Application number: JP2003508341A
Authority: JP
Filing date: 2002-07-01
Publication date: 2005-12-22
Anticipated expiration: 2022-07-01

Claims

A sustained release device comprising a number of sustained release mini-implants or pellets;
A pharmaceutically active composition in which each mini-implant is carried in or on a sustained release support material;
Including
A pharmaceutically active composition at least one pharmaceutically active ingredient; and a carrier thereof;
Including
Mini-implants or pellets where each implant is of insufficient size and / or loading to provide a predetermined desired threshold blood level of the pharmaceutically active ingredient for treatment of the selected indication individually Provides a zero order release of the pharmaceutically active ingredient;
A sustained release device, wherein in use, the sustained release device provides a zero order release of the pharmaceutically active ingredient above a predetermined desired threshold level of pharmaceutically active ingredient for treatment of a selected indication.

The sustained release device according to claim 1, wherein each mini-implant is of an uncoated or coated rod or matrix type.

Each mini-implant
An inner layer containing a pharmaceutically active ingredient; and an impermeable outer layer;
The sustained release device according to claim 2, comprising:

4. Each mini-implant takes the form of an extruded rod bearing an impermeable coating thereon, wherein the impermeable coating is formed from a liquid coating composition comprising a liquid siloxane component. The sustained release device described.

Each mini-implant is about 0.1 to 0.5 times the length of a single rod-shaped implant that can provide a desired threshold blood level, depending on the pharmaceutically active ingredient selected. The sustained release device according to claim 1.

Depending on the pharmaceutically active ingredient selected, each mini-implant can provide a desired threshold blood level of about 0.20 to 0.50 of the length and / or diameter of a single rod-shaped implant. 6. The sustained release device according to claim 5, which is doubled.

The sustained release mini-implant is of a generally cylindrical structure having a cross-sectional diameter of about 0.2-15 mm and an axial length of about 0.2-7.5 mm. Slow release device.

The sustained release device according to claim 7, wherein the axial length of the mini-implant is about 0.5 to 5 mm.

Mini implants or pellets
At a first size providing a blood level of the pharmaceutically active ingredient of about 1.25 to 3 times the desired threshold blood level for a first relatively short period; and for a second longer period of a desired threshold A second size that provides a blood level of the pharmaceutically active ingredient at or near the blood level,
The sustained release device according to claim 1 provided.

10. The sustained release device of claim 9, wherein the first period is about 1-4 weeks and the second period is about 4-52 weeks.

A pharmaceutically active composition is an acetone preparation, an anabolic agent, an anesthetic, an analgesic, an antacid, an anti-arthritic agent, an antibody, an anticonvulsant, an antibacterial agent, an antihistamine, an anti-infective agent, an anti-inflammatory agent Antimicrobial agents, antiparasitic agents, antiprotozoal agents, anti-ulcer agents, antiviral agents, behavioral improvers, biologics, blood and blood substitutes, bronchodilators and expectorants, cancer drugs and related drugs, heart Vascular drugs, central nervous system drugs, coccidial deterrents and anti-coccidial drugs, contraceptives, contrast agents, antidiabetics, diuretics, ovulation promoters, growth hormones, growth promoters, hematopoietics, hemostatics, hormone replacement therapy, Hormones and analogs, immunostimulants, minerals, muscle relaxants, natural products, dietary supplements and nutrients, obesity drugs, eye drops, osteoporosis drugs, analgesics, peptides and polypeptides, respiratory drugs, analgesics And mental stability , The product of grafting, urinary oxidizing agent, comprising the active ingredient at least one pharmaceutically selected from the vaccine and adjuvant and the group consisting of vitamins, sustained release apparatus according to claim 1.

12. The sustained release device according to claim 11, wherein the pharmaceutically active ingredient comprises an antiparasitic agent that is a macrocyclic lactone, an insect growth regulator, or a mixture thereof.

The sustained release device according to claim 12, wherein the macrocyclic lactone component comprises ivermectin.

The sustained release device according to claim 1, wherein the pharmaceutical carrier is selected to allow release of the pharmaceutically active ingredient from the composition over an extended period of time.

15. The sustained release device according to claim 14, wherein the pharmaceutical carrier comprises a water soluble substance that is solid at the body temperature of the animal or human to which it is administered in a pharmaceutically active composition.

16. The sustained release device according to claim 15, wherein the pharmaceutical carrier is selected from one or more of the group consisting of synthetic polymers, saccharides, amino acids, inorganic salts, organic salts and proteins.

The sustained release device according to claim 16, wherein the pharmaceutical carrier is a saccharide or an inorganic salt or a mixture thereof.

The pharmaceutically active composition comprises a lipophilic medicament and the pharmaceutical carrier is one or more of polyethylene glycol, polyoxystearate 40, polyoxyethylene polyoxypropylene glycol, sucrose ester of fatty acid, sodium lauryl sulfate, sodium oleate 18. The sustained release device according to claim 17, comprising one or more amphiphiles selected from the group consisting of sodium chloride and sodium desoxycholate.

19. The sustained release device according to claim 18, wherein the carrier comprises polyoxyethylene polyoxypropylene glycol, sucrose, sodium chloride, or sodium desoxycholate, or a mixture of two or more thereof.

15. The sustained release device according to claim 14, wherein the pharmaceutical carrier constitutes about 10% to 30% by weight, based on the total weight of the pharmaceutically active composition.

The sustained release support is in the form of a support matrix, tablet or rod formed from a biocompatible material selected from the group consisting of polyester, polyamino acid, silicon, ethylene vinyl acetate copolymer, polyglycerol sebacic acid and polyvinyl alcohol. The sustained release device according to claim 1.

The sustained release device according to claim 21, wherein the sustained release support material comprises a silicon material.

23. The sustained release device of claim 22, wherein the silicone material is formed from a methyl-vinylsiloxane polymer that includes fumed silica as a reinforcing filler.

A sustained release kit comprising a number of sustained release mini-implants or pellets packaged for delivery of a single treatment,
Each mini-implant
At least one pharmaceutically active ingredient; and its carrier;
A pharmaceutically active composition comprising: a sustained release support;
A pharmaceutically active composition is carried in or on a sustained release support material,
Each implant is of a size and / or loading that is insufficient to individually provide a predetermined desired threshold blood level of the pharmaceutically active ingredient for treatment of the selected indication;
A kit wherein the size of the mini-implant or pellet provides a zero order release of the pharmaceutically active ingredient.

Mini implants or pellets
At a first size providing a blood level of the pharmaceutically active ingredient of about 1.25 to 3 times the desired threshold blood level for a first relatively short period; and for a second longer period of a desired threshold A second size that provides a blood level of the pharmaceutically active ingredient at or near the blood level,
25. A sustained release kit according to claim 24 provided.

Each mini-implant
An inner layer containing a pharmaceutically active ingredient; and an impermeable outer layer;
The sustained release kit according to claim 24, comprising:

25. The sustained release kit of claim 24, wherein a plurality of sustained release mini-implants are encased within a biodegradable sheath.

25. The sustained release kit of claim 24 further comprising a delivery device comprising an injection device for subcutaneous or intramuscular delivery of the implant.

A method for the therapeutic or prophylactic treatment of a disease state of an animal (including human) in need of treatment, comprising administering to the animal a slow broadcast delivery device comprising a number of sustained release mini-implants or pellets Including:
Each mini-implant
At least one pharmaceutically active ingredient; and its carrier;
A pharmaceutically active composition comprising: a sustained release support;
A pharmaceutically active composition is carried in or on a sustained release support material,
Each implant is of insufficient size to individually provide a predetermined desired threshold blood level of a pharmaceutically active ingredient for treatment of the selected disease indication;
A method wherein the size of the mini-implant or pellet provides a zero order release of the pharmaceutically active ingredient.

Mini implants or pellets
At a first size providing a blood level of the pharmaceutically active ingredient of about 1.25 to 3 times the desired threshold blood level for a first relatively short period; and for a second longer period of a desired threshold A second size that provides a blood level of the pharmaceutically active ingredient at or near the blood level,
30. The method of claim 29, provided.